AR101505A1 - THERAPEUTIC COMBINATIONS OF A BTK INHIBITOR, A PI3K INHIBITOR, A JAK-2 INHIBITOR, AND / OR A BCL-2 INHIBITOR - Google Patents

THERAPEUTIC COMBINATIONS OF A BTK INHIBITOR, A PI3K INHIBITOR, A JAK-2 INHIBITOR, AND / OR A BCL-2 INHIBITOR

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Publication number
AR101505A1
AR101505A1 ARP150102592A ARP150102592A AR101505A1 AR 101505 A1 AR101505 A1 AR 101505A1 AR P150102592 A ARP150102592 A AR P150102592A AR P150102592 A ARP150102592 A AR P150102592A AR 101505 A1 AR101505 A1 AR 101505A1
Authority
AR
Argentina
Prior art keywords
inhibitor
cells
btk
pi3k
pharmaceutically acceptable
Prior art date
Application number
ARP150102592A
Other languages
Spanish (es)
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Acerta Pharma Bv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Acerta Pharma Bv filed Critical Acerta Pharma Bv
Publication of AR101505A1 publication Critical patent/AR101505A1/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Combinaciones terapéuticas de un inhibidor de una fosfoinositida 3-quinasa (PI3K), incluyendo inhibidores de PI3K selectivos de las isoformas g y d y selectivos tanto de las isoformas g como d (PI3K-g,d, PI3K-g y Pl3K-d), un inhibidor de Janus quinasa-2 (JAK-2), un inhibidor de la tirosina quinasa de Bruton (BTK) y/o un inhibidor del linfoma 2 de células B (BCL-2). Combinaciones terapéuticas de un inhibidor de PI3K-d y un inhibidor de BTK, un inhibidor de JAK-2 y un inhibidor de BTK y un inhibidor de BCL-2 y BTK. Reivindicación 7: El método de acuerdo con una de las reivindicaciones 1 a 6, en donde el inhibidor de BTK es la fórmula (1), o una de sus sales, cocristales, hidratos, solvatos o profármacos farmacéuticamente aceptables. Reivindicación 8: El método de acuerdo con una de las reivindicaciones 1 a 6, en donde el inhibidor de BTK se selecciona del grupo que consiste en: el grupo de fórmulas (2), y sus sales, cocristales, hidratos, solvatos o profármacos farmacéuticamente aceptables. Reivindicación 9: El método de acuerdo con una de las reivindicaciones 1 a 8, en donde el inhibidor de BCL-2 es de fórmula (3), o una de sus sales, cocristales, hidratos, solvatos o profármacos farmacéuticamente aceptables. Reivindicación 13: El método de acuerdo con una de las reivindicaciones 2, 3 ó 10 - 12, en donde el inhibidor de PI3K se selecciona del grupo que consiste en: el grupo de fórmulas (4), y sus sales, solvatos, hidratos, cocristales o profármacos farmacéuticamente aceptables. Reivindicación 15: El método de acuerdo con la reivindicación 14, en donde el inhibidor de JAK-2 se selecciona del grupo que consiste en los compuestos de fórmulas (5), de fórmula (6), y sus sales, cocristales, hidratos, solvatos o profármacos farmacéuticamente aceptables. Reivindicación 16: El método de acuerdo con una de las reivindicaciones 1 a 15, en donde el método también comprende la etapa de administración de una cantidad terapéuticamente efectiva de un anticuerpo anti-CD20 seleccionado del grupo que consiste en rituximab, obinutuzumab, ofatumumab, veltuzumab, tositumomab, ibritumomab y sus fragmentos, derivados, conjugados, variantes, complejos rotulados con radioisótopos y biosimilares. Reivindicación 19: El método de acuerdo con la reivindicación 18, que también comprende la etapa de administración de una dosis terapéuticamente efectiva de gemcitabina. Reivindicación 20: El método de acuerdo con una de las reivindicaciones 18 a 19, que también comprende la etapa de administración de una dosis terapéuticamente efectiva de paclitaxel ligado a albúmina. Reivindicación 51: Una composición que comprende (i) a inhibidor de linfoma de células B 2 (BLC-2) o una de sus sales, solvatos, hidratos, cocristales o profármacos farmacéuticamente aceptables y (ii) un inhibidor de la tirosina quinasa de Bruton (BTK) o una de sus sales, solvatos, hidratos, cocristales o profármacos farmacéuticamente aceptables, para usar en el tratamiento de un cáncer de tumor sólido, en donde (i) y (ii) son cada uno proporcionados en una dosis efectiva para inhibir la señalización entre las células del cáncer de tumor sólido y al menos un microambiente tumoral seleccionado del grupo que consiste en macrófagos, monocitos, mastocitos, células T helper, células T citotóxicas, células T regulatorias, células natural killer, células supresoras derivadas de mieloides, células B reguladoras, neutrófilos, células dendríticas y fibroblastos. Reivindicación 61: La composición de acuerdo con una de las reivindicaciones 58 a 60, que también comprende una dosis terapéuticamente efectiva de un ingrediente farmacéutico activo anticoagulante o antiplaquetario.Therapeutic combinations of a phosphoinositide 3-kinase (PI3K) inhibitor, including selective PI3K inhibitors of the gydy isoforms selective of both the g and d isoforms (PI3K-g, d, PI3K-g and Pl3K-d), an inhibitor of Janus kinase-2 (JAK-2), a Bruton tyrosine kinase inhibitor (BTK) and / or a B-cell lymphoma 2 inhibitor (BCL-2). Therapeutic combinations of a PI3K-d inhibitor and a BTK inhibitor, a JAK-2 inhibitor and a BTK inhibitor and an inhibitor of BCL-2 and BTK. Claim 7: The method according to one of claims 1 to 6, wherein the BTK inhibitor is the formula (1), or one of its pharmaceutically acceptable salts, co-crystals, hydrates, solvates or prodrugs. Claim 8: The method according to one of claims 1 to 6, wherein the BTK inhibitor is selected from the group consisting of: the group of formulas (2), and their pharmaceutically acceptable salts, co-crystals, hydrates, solvates or prodrugs. acceptable. Claim 9: The method according to one of claims 1 to 8, wherein the BCL-2 inhibitor is of formula (3), or one of its pharmaceutically acceptable salts, co-crystals, hydrates, solvates or prodrugs. Claim 13: The method according to one of claims 2, 3 or 10-12, wherein the PI3K inhibitor is selected from the group consisting of: the group of formulas (4), and their salts, solvates, hydrates, pharmaceutically acceptable co-crystals or prodrugs. Claim 15: The method according to claim 14, wherein the JAK-2 inhibitor is selected from the group consisting of the compounds of formulas (5), of formula (6), and their salts, co-crystals, hydrates, solvates or pharmaceutically acceptable prodrugs. Claim 16: The method according to one of claims 1 to 15, wherein the method also comprises the step of administering a therapeutically effective amount of an anti-CD20 antibody selected from the group consisting of rituximab, obinutuzumab, ofatumumab, veltuzumab , tositumomab, ibritumomab and its fragments, derivatives, conjugates, variants, complexes labeled with radioisotopes and biosimilars. Claim 19: The method according to claim 18, which also comprises the step of administering a therapeutically effective dose of gemcitabine. Claim 20: The method according to one of claims 18 to 19, which also comprises the step of administering a therapeutically effective dose of paclitaxel bound to albumin. Claim 51: A composition comprising (i) a B 2 cell lymphoma inhibitor (BLC-2) or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal or prodrug and (ii) a Bruton tyrosine kinase inhibitor (BTK) or one of its pharmaceutically acceptable salts, solvates, hydrates, co-crystals or prodrugs, for use in the treatment of solid tumor cancer, where (i) and (ii) are each provided in an effective dose to inhibit signaling between solid tumor cancer cells and at least one tumor microenvironment selected from the group consisting of macrophages, monocytes, mast cells, helper T cells, cytotoxic T cells, regulatory T cells, natural killer cells, myeloid-derived suppressor cells, regulatory B cells, neutrophils, dendritic cells and fibroblasts. Claim 61: The composition according to one of claims 58 to 60, which also comprises a therapeutically effective dose of an anticoagulant or antiplatelet active pharmaceutical ingredient.

ARP150102592A 2014-08-11 2015-08-11 THERAPEUTIC COMBINATIONS OF A BTK INHIBITOR, A PI3K INHIBITOR, A JAK-2 INHIBITOR, AND / OR A BCL-2 INHIBITOR AR101505A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462035795P 2014-08-11 2014-08-11

Publications (1)

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AR101505A1 true AR101505A1 (en) 2016-12-21

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ARP150102592A AR101505A1 (en) 2014-08-11 2015-08-11 THERAPEUTIC COMBINATIONS OF A BTK INHIBITOR, A PI3K INHIBITOR, A JAK-2 INHIBITOR, AND / OR A BCL-2 INHIBITOR

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AR (1) AR101505A1 (en)
MA (1) MA40596B1 (en)

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MA40596B1 (en) 2021-12-31
MA40596A (en) 2021-05-05

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